Nisoldipine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Angina pectoris; HTN Immediate-release: Initial: 5 or 10 mg bid increased if necessary at intervals of no less than 1 wk to max of 20 mg bid. Modified-release: Initial: 17 mg once daily, increased by 8.5 mg/wk (or longer intervals). Max: 34 mg once daily.
Dosage Details
Oral
Angina pectoris, Hypertension
Adult: Immediate-release: Initially, 5 or 10 mg bid increased if necessary at intervals of no less than 1 wk to max of 20 mg bid. Modified-release: Initially, 17 mg once daily, increased by 8.5 mg/wk (or longer intervals). Max: 34 mg once daily.
Elderly: Immediate-release: Initially, 5 or 10 mg once daily. Modified-release: Initially, 8.5 mg once daily.
Hepatic Impairment
Immediate-release: Initially, 5 or 10 mg once daily. Modified-release: Initially, 8.5 mg once daily.
Contraindications
Concomitant use w/ CYP3A4 inducers.
Special Precautions
Patients w/ severe aortic stenosis, heart failure, hypertrophic cardiomyopathy (HCM) w/ outflow tract obstruction. Hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Dizziness, headache, peripheral oedema, chest pain, angina exacerbation, palpitations, vasodilation, pharyngitis, sinusitis, nausea, rash.
MonitoringParameters
Monitor BP carefully during the initial admin or if there is subsequent upward dose adjustment.
Overdosage
Symptoms: Hypotension. Management: Symptomatic and supportive treatment. Monitor CV and resp function. Elevation of extremities, use of Ca infusion, pressor agents and fluid may be necessary.
Drug Interactions
May increase serum levels w/ CYP3A4 inhibitors. Increased levels w/ cimetidine. Increased antihypertensive effect w/ atenolol. Propranolol attenuated heart rate increase following intake of immediate-release nisoldipine. Reduced bioavailability w/ quinidine. Increased quinidine levels w/ immediate-release nisoldipine.
Potentially Fatal: Concomitant use w/ potent CYP3A4 inducers (e.g. phenytoin) may decrease nisoldipine plasma concentration to undetectable levels.
Food Interaction
High-fat food increases peak concentration. Avoid grapefruit-containing foods and beverages as it increases peak concentrations and oral bioavailability of nisoldipine. Levels may be reduced w/ St John's wort.
Action
Description: Nisoldipine is a dihydropyridine Ca channel blocker. It inhibits the movement of Ca ions into vascular smooth muscle and cardiac muscle. It reversibly competes w/ other dihydropyridines for binding to the Ca channel.
Duration: >24 hr.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. High-fat food increases peak concentration. Bioavailability: Approx 4-8%.
Distribution: Plasma protein binding: >99%.
Metabolism: Undergoes rapid and extensive first-pass metabolism in the gut wall and liver.
Excretion: Via urine (approx 60-80%) and faeces (remaining dose as metabolites). Terminal elimination half-life: Approx 7-12 hr.
Storage
Store between 20-25°C. Protect from light and moisture.
MIMS Class
Disclaimer: This information is independently developed by MIMS based on Nisoldipine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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